Bombesin GastrinReleasing Peptide Luteinizing Releasing Hormone Receptor Subtypes and Luteinizing Hormone Receptor

Bombesin/gastrin-releasing peptide (GRP) and luteinizing-releasing hormone (LHRH) receptor subtypes have been detected in a variety of human malignancies.31 The presence of these peptidergic receptors permits the localization of certain primary tumors and their metastasis using radiolabeled and bombesin analogs. Cyto-toxic analogs of bombesin and LH, a hybrid consisting of a radical conjugated to a peptide carrier, target these tumors and appear promising in the treatment of a variety of cancers including small cell lung carcinomas, prostate, ovarian, and gastrointestinal cancers, and brain tumors expressing the respective receptors.31 The preclinical work with these cytotoxic conjugates is continuing and clinical trials are pending.

A large number of naturally occurring mutations within the LH receptor, all displaying constitutive activity, have been associated with onset of familial or sporadic precocious puberty and Leydig cell hyperplasia. One mutation that is somatic in nature (D578H in transmembrane helix 6) is found in Leydig cell tumors of boys with precocious puberty.33-35

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